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Chinese Journal of Polymer Science 2010年第5期28卷 731-743页

作者： Abdol-reza Hajipour Sakineh Habibi Arnold E.Ruoho dept.of pharmacology University of WisconsinMedical SchoolMadison53706-1532WIUSA Pharmaceutical Research Laboratory College of ChemistryIsfahan University of TechnologyIsfahan 84156IR Iran

A novel calix[4]arene derivative 2 with amino functional groups at the lower rim was first prepared via introduction of nitro functional groups and amination of the dinitro derivative of calix[4]arene. The optically active monomers were synthesized by dehydration of L-leucine （and L-isoleucine） and 3,3＇,4,4＇-benzophenonetetracarboxylic- 3,3＇,4,4＇-dianhydride （3） followed by reaction with thionyl chloride to form 5a and 5b. Two methods, polymerization under microwave irradiation and solution polymerization in CH2Cl2/TEA, were then employed to carry out the condensation polymerization of 2 with the optically active monomers 5a and 5b, respectively. The polymerization conditions affected the kind of resulting polymers, poly（amide-imide）s （PAIs） 6a and 6b and poly（ester-imide）s （PEIs） 6a＇ and 6b＇ were obtained selectively in good yields and moderate inherent viscosities. Sorption-extraction experiments were carried out using cram picrate extraction method and verified good binding ability of the resulting calixarene-based polymers towards silver, alkali metal and toxic heavy metal cations. Also thermogravimetric analysis indicated that the resulting PAIs and PEIs were thermally stable.

关键词： Condensation polymerization Ionophores Optically active Toxic heavy metals Polymeric calixarenes Thermal stability.

Regulation of expression of drug-metabolizing enzymes by oncogenic signaling pathways in liver tumors: a review

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Acta Pharmaceutica Sinica B 2020年第1期10卷 113-122页

作者： Albert Braeuning Michael Schwarz German Federal Institute for Risk Assessment Dept.Food SafetyBerlin 10589Germany Eberhard Karls University of Tu¨bingen Inst.of Pharmacology and ToxicologyDept.of ToxicologyTu¨bingen 72074Germany

Mutations in genes encoding key players in oncogenic signaling pathways trigger specific downstream gene expression profiles in the respective tumor cell *** regulation of genes related to cell growth,survival,and death has been extensively studied,much less is known on the regulation of drug-metabolizing enzymes(DMEs)by oncogenic ***,a comprehensive review of the available literature is presented summarizing the impact of the most relevant genetic alterations in human and rodent liver tumors on the expression of DMEs with a focus on phasesⅠandⅡof xenobiotic *** few data are available with respect to DME regulation by p53-dependent signaling,telomerase expression or altered chromatin *** contrast,DME regulation by constitutive activation of oncogenic signaling via the RAS/RAF/mitogen-activated protein kinase(MAPK)cascade or via the canonical WNT/β-catenin signaling pathway has been analyzed in greater depth,demonstrating mostly positive-regulatory effects of WNT/β-catenin signaling and negativeregulatory effects of MAPK *** studies have revealed molecular interactions between oncogenic signaling and nuclear xeno-sensing receptors which underlie the observed alterations in DME expression in liver *** of altered DME expression and inducibility in liver tumors with a specific gene expression profile may impact pharmacological treatment options.

关键词： Xenobiotic metabolism Hepatocytes WNT/b-catenin signaling RAS/MAPK signaling Gene mutation Cytochrome P450

PHARMACOLOGICAL RESEARCH ON THE EFFECT OF LICORICE

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Journal of Traditional Chinese Medicine 1988年第4期8卷 307-309页

作者：任骏王振钢 dept.of pharmacology Peking Union Medical College

Licorice is extracted from the roots and sto-lons of Glycyrrhiza uralensis Fisch,a plant initial-ly cultivated for its medical value as describedvery early in“Compendium of Materia Medica”(Li Shizhen).In 1760 a certain George Dunhilladded sugar to licorice,creating a popular *** is widely used as a flavoringagent in foods,beverages,tobacco and some *** studies of its effective com-ponents and mechanisms of action have beenmade only recently,however,with the develop-ment of modem medical techniques.

关键词： PHARMACOLOGICAL RESEARCH ON THE EFFECT OF LICORICE AIDS

ROLE OF TRPV1 RECEPTORS IN BLEOMYCIN-INDUCED SCLERO-DERMA IN MICE

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ROLE OF TRPV1 RECEPTORS IN BLEOMYCIN-INDUCED SCLERO-DERMA IN...

第十五届国际药理学大会

作者： Szabo Arpad Czirjak Laszlo Helyes Zsuzsanna Laszlo Terezia Elekes Krisztian Starr Anna Brain Susan Szolcsanyi Janos Pinter Erika dept.of pharmacology University of PecsHungary dept.of Immunology and Rheumatology University of PecsHungary dept.of pharmacology University of PecsHungary dept.of Phatology University of PecsHungary dept.of pharmacology University of PecsHungary Centre of Cardiovascular Biology and Medicine Kings CollegeUK Centre of Cardiovascular Biology and Medicine Kings CollegeUK dept.of pharmacology University of PecsHungary dept.of pharmacology University of PecsHungary

＜正＞ Neuropeptides released from the activated capsaicin-sensitive. TRPV1 receptor-expressing sensory nerves modulate inflammatory processes. This study examines the role of TRPV1 and calcitonin-gene related peptide（ CGRP） in bleomycin-induced scleroderma using transgenic *** sclerosis of TRPV1 receptor and CGRP gene-deficient mice （TRPV1-/-and CGRP-/-） and their wild-type （WT） counterparts was induced by daily s. c. bleomycin injection during 30 days. Composite histological sclerosis score was calculated on the basis of thickening, leukocyte infiltration and amount of collagen boundles. The collagen-specific amino-acid, hydroxyproline. in the skin was measured with spectrophotometry. Quantitative real-time RT-PCR was used to determine type Ⅰ collagen-alpha mRNA. Bleomycin induced a marked skin thickening and fibrosis. Both sclerosis score and hydroxyproline content of the skin were significantly increased in TRPV1-/-and CGRP-/-mice compared to WT animals. Type Ⅰ collagenalpha mRNA was significantly higher in bleomycin-treated TRPV1-/-mice. These data suggest that CGRP released by TRPV1 activation exerts a protective action against fibrosis.

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Interaction between muscarinic and β-adrenergic receptors

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Interaction between muscarinic and β-adrenergic receptors

中国药理学会生化与分子药理学专业委员会网络药理学研讨会

作者： Martin C.Michel dept.of pharmacology University of MainzMainzGermany

＜正＞In many tissues the parasympathetic and sympathetic nervous system regulate smooth muscle tone via their transmitters acetylcholine and noradrenaline,*** smooth muscle effects of acetylcholine via muscarinic rec...

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The involvement of central cholinergic system in the analgesic effect of intracerebroventricularly injected CDPcholine in acute pain models of rats

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The involvement of central cholinergic system in the analges...

第十五届国际药理学大会

作者： HAMURTEKIN EMRE GURUN MINE SIBEL Uludag Univ Medical FacultyDept.of Pharmacology16059Bursa/TURKEY Uludag Univ Medical FacultyDept.of Pharmacology16059Bursa/TURKEY

＜正＞ In the present study,intracerebroventricularly injected CDP-choline （0.5, 1, 2 micromoles） induced dose and time dependent antinociceptive effects in thermal and mechanical paw withdrawal tests and acetic acid writhing tests in rats. E-quimolar dose of CDP- choline （imicromole） and choline （imicromole） caused similar antinociceptive effects while cytidine （Imicromole） produced small,transient but statically significant antinociceptive effect. Mecamylamine, MLA and HC - 3 pretreatments completely antagonized CDP - choline induced antinocicep-tion in acute thermal and mechanical tests while HC - 3. MLA. mecamylamine and atropine pretreatments partially blocked the antinociceptive effect of CDP -choline in the acetic acid writhing test. CDPcholine did not impair motor performance of rats evaluated by rota - rod test. These results indicate that centrally administered CDP - choline induced dose and time dependent antinociception in rats by activating mainly central cholinergic nicotinic receptors through the activation of presynaptic cholinergic mechanisms.

关键词： CDP-choline antinociception acute pain cholinergic

Identification of Anxiolytic Potential of Niranthin:In-vivo and Computational Investigations

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Natural Products and Bioprospecting 2021年第2期11卷 223-233页

作者： Atul R.Chopade Prakash M.Somade Pratik P.Somade Suraj N.Mali Department of pharmacology Rajarambapu College of PharmacyKasegaonSangliMaharashtra 415404India dept.of Physiology Krishna Institute of Medical SciencesKaradMaharashtraIndia Government College of Pharmacy KaradMaharashtraIndia

Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and *** is a lignan isolated from various Phyllanthus *** literature survey on niranthin highlights wide ranges of the therapeutic *** a present study,based on our previous investigations,we evaluated pure,isolated and characterized niranthin as an anxiolytic *** niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole]was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test(EPM)and Light&Dark Exploration test(L&D).GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM *** docking simulation studies(pdb id:4COF)carried out by Vlife QSAR software showed that niranthin(docking score:−62.1714 kcal/mol)have shown comparatively best docking score compared to the standard drug Diazepam(docking score:−63.1568 kcal/mol).To conclude,Niranthin has probable potential in the management of anxiety *** in-silico and in-vivo analysis(indirectly)indicated the plausible role of GABA mediation for anxiolytic ***,these studies are preliminary,future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.

关键词： pharmacology Phytoconstituents Niranthin Lignan Anxiolytic activity EPM models

Regulation,Structure and Function of Aquaporin

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Regulation,Structure and Function of Aquaporin

2008心血管药理学术研讨会

作者： Masato Yasui dept.of pharmacology School of MedicineKeio UniversityTokyoJapan

The discovery of the water channel aquaporin has greatly expanded our understanding of the regulation of the water permeability of biological *** atomic structure of aquaporin-1 (AQP1)demonstrated how aquaporin is fre...

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Functional calsequestrin-1 exists in heart and is involved in the malignant hyperthermia-like arrhythmias

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Functional calsequestrin-1 exists in heart and is involved i...

首届东方药理论坛暨2018年全国心脑血管药理学术会议、上海市药理学会第十九届学术年会

作者： Dali LUO Zhipeng SUN Yutong YANG Yi MA dept.of pharmacology Basic Medical SchoolCapital Medical University

Arrhythmias are early symptom in patient with malignant hyperthermia （MH）.Although it is well established that loss-of-function mutation in calsequestrinl （Casql）is one of the important cause of MH,leading to an abnormal Ca2+release and MH attack in skeletal muscle,it is still unclear about the mechanism underlying MH-arrhythmias,for Casq2 is the only functional subtype found in myocardial

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Initiation of Cellular Senescence and Metabolic Regulation

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Initiation of Cellular Senescence and Metabolic Regulation

中国生物化学与分子生物学会2016年全国学术会议

作者： Lifeng Yuan Xiao-Fan Wang dept.of pharmacology and Cancer Biology Duke University Medical Center

Cellular senescence is a state of irreversible arrest of cell proliferation in which cells remain viable and metabolically *** cell fate has been recognized as a vital barrier to tumorigenesis and may also be involved in the processes of embryonic development and *** signaling pathways including the p53/p21 and INK4a/p RB network are known to be involved in cellular ***,

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